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Application of fragment screening and fragment linking to the discovery of novel thrombin inhibitors. [electronic resource] by
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- Blakemore, Wendy
- Chessari, Gianni
- Congreve, Miles
- Howard, Steven
- Jhoti, Harren
- Murray, Christopher W
- Seavers, Lisa C A
- van Montfort, Rob L M
Producer: 20060410
In:
Journal of medicinal chemistry vol. 49
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22.
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Identification of autophosphorylation inhibitors of the inositol-requiring enzyme 1 alpha (IRE1α) by high-throughput screening using a DELFIA assay. [electronic resource] by
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- Hardcastle, Anthea
- McAndrew, P Craig
- Strover, Jade A
- Mirza, Amin
- Morgan, Gareth J
- Burke, Rosemary
- Davies, Faith E
- Collins, Ian
- van Montfort, Rob L M
Producer: 20131118
In:
Journal of biomolecular screening vol. 18
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23.
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Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70. [electronic resource] by
- Cheeseman, Matthew D
- Westwood, Isaac M
- Barbeau, Olivier
- Rowlands, Martin
- Dobson, Sarah
- Jones, Alan M
- Jeganathan, Fiona
- Burke, Rosemary
- Kadi, Nadia
- Workman, Paul
- Collins, Ian
- van Montfort, Rob L M
- Jones, Keith
Producer: 20170529
In:
Journal of medicinal chemistry vol. 59
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Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. [electronic resource] by
- Gurden, Mark D
- Westwood, Isaac M
- Faisal, Amir
- Naud, Sébastien
- Cheung, Kwai-Ming J
- McAndrew, Craig
- Wood, Amy
- Schmitt, Jessica
- Boxall, Kathy
- Mak, Grace
- Workman, Paul
- Burke, Rosemary
- Hoelder, Swen
- Blagg, Julian
- Van Montfort, Rob L M
- Linardopoulos, Spiros
Producer: 20151124
In:
Cancer research vol. 75
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Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization. [electronic resource] by
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- Taylor, Dawn
- Thomson, Douglas W
- Cheung, Kwai-Ming J
- Boxall, Kathy
- Mas-Droux, Corine
- Barillari, Caterina
- Burns, Samantha
- Grummitt, Charles G
- Collins, Ian
- van Montfort, Rob L M
- Aherne, G Wynne
- Bayliss, Richard
- Hoelder, Swen
Producer: 20101228
In:
Journal of medicinal chemistry vol. 53
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26.
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Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2. [electronic resource] by
- Silva-Santisteban, M Cris
- Westwood, Isaac M
- Boxall, Kathy
- Brown, Nathan
- Peacock, Sam
- McAndrew, Craig
- Barrie, Elaine
- Richards, Meirion
- Mirza, Amin
- Oliver, Antony W
- Burke, Rosemary
- Hoelder, Swen
- Jones, Keith
- Aherne, G Wynne
- Blagg, Julian
- Collins, Ian
- Garrett, Michelle D
- van Montfort, Rob L M
Producer: 20140123
In:
PloS one vol. 8
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A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms. [electronic resource] by
- Jones, Alan M
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- Matthews, Thomas P
- Cheeseman, Matthew D
- Rowlands, Martin G
- Jeganathan, Fiona
- Burke, Rosemary
- Lee, Diane
- Kadi, Nadia
- Liu, Manjuan
- Richards, Meirion
- McAndrew, Craig
- Yahya, Norhakim
- Dobson, Sarah E
- Jones, Keith
- Workman, Paul
- Collins, Ian
- van Montfort, Rob L M
Producer: 20180619
In:
Scientific reports vol. 6
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The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design. [electronic resource] by
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- Cano, Celine
- Travers, Jon
- Boxall, Kathy
- Chow, Chiau Ling
- Burns, Sam
- Schmitt, Jessica
- Pickard, Lisa
- Barillari, Caterina
- McAndrew, P Craig
- Clarke, Paul A
- Linardopoulos, Spiros
- Griffin, Roger J
- Aherne, G Wynne
- Raynaud, Florence I
- Workman, Paul
- Jones, Keith
- van Montfort, Rob L M
Producer: 20140722
In:
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Privileged Structures and Polypharmacology within and between Protein Families. [electronic resource] by
- Meyers, Joshua
- Chessum, Nicola E A
- Ali, Salyha
- Mok, N Yi
- Wilding, Birgit
- Pasqua, A Elisa
- Rowlands, Martin
- Tucker, Michael J
- Evans, Lindsay E
- Rye, Carl S
- O'Fee, Lisa
- Le Bihan, Yann-Vaï
- Burke, Rosemary
- Carter, Michael
- Workman, Paul
- Blagg, Julian
- Brown, Nathan
- van Montfort, Rob L M
- Jones, Keith
- Cheeseman, Matthew D
Publication details: ACS medicinal chemistry letters Dec 2018
In:
ACS medicinal chemistry letters vol. 9
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High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers. [electronic resource] by
- Anderhub, Simon J
- Mak, Grace Wing-Yan
- Gurden, Mark D
- Faisal, Amir
- Drosopoulos, Konstantinos
- Walsh, Katie
- Woodward, Hannah L
- Innocenti, Paolo
- Westwood, Isaac M
- Naud, Sébastien
- Hayes, Angela
- Theofani, Efthymia
- Filosto, Simone
- Saville, Harry
- Burke, Rosemary
- van Montfort, Rob L M
- Raynaud, Florence I
- Blagg, Julian
- Hoelder, Swen
- Eccles, Suzanne A
- Linardopoulos, Spiros
Producer: 20200609
In:
Molecular cancer therapeutics vol. 18
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Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives. [electronic resource] by
- Tisi, Dominic
- Chiarparin, Elisabetta
- Tamanini, Emiliano
- Pathuri, Puja
- Coyle, Joseph E
- Hold, Adam
- Holding, Finn P
- Amin, Nader
- Martin, Agnes C L
- Rich, Sharna J
- Berdini, Valerio
- Yon, Jeff
- Acklam, Paul
- Burke, Rosemary
- Drouin, Ludovic
- Harmer, Jenny E
- Jeganathan, Fiona
- van Montfort, Rob L M
- Newbatt, Yvette
- Tortorici, Marcello
- Westlake, Maura
- Wood, Amy
- Hoelder, Swen
- Heightman, Tom D
Producer: 20170622
In:
ACS chemical biology vol. 11
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Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen. [electronic resource] by
- Cheeseman, Matthew D
- Chessum, Nicola E A
- Rye, Carl S
- Pasqua, A Elisa
- Tucker, Michael J
- Wilding, Birgit
- Evans, Lindsay E
- Lepri, Susan
- Richards, Meirion
- Sharp, Swee Y
- Ali, Salyha
- Rowlands, Martin
- O'Fee, Lisa
- Miah, Asadh
- Hayes, Angela
- Henley, Alan T
- Powers, Marissa
- Te Poele, Robert
- De Billy, Emmanuel
- Pellegrino, Loredana
- Raynaud, Florence
- Burke, Rosemary
- van Montfort, Rob L M
- Eccles, Suzanne A
- Workman, Paul
- Jones, Keith
Producer: 20170807
In:
Journal of medicinal chemistry vol. 60
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Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). [electronic resource] by
- Naud, Sébastien
- Westwood, Isaac M
- Faisal, Amir
- Sheldrake, Peter
- Bavetsias, Vassilios
- Atrash, Butrus
- Cheung, Kwai-Ming J
- Liu, Manjuan
- Hayes, Angela
- Schmitt, Jessica
- Wood, Amy
- Choi, Vanessa
- Boxall, Kathy
- Mak, Grace
- Gurden, Mark
- Valenti, Melanie
- de Haven Brandon, Alexis
- Henley, Alan
- Baker, Ross
- McAndrew, Craig
- Matijssen, Berry
- Burke, Rosemary
- Hoelder, Swen
- Eccles, Suzanne A
- Raynaud, Florence I
- Linardopoulos, Spiros
- van Montfort, Rob L M
- Blagg, Julian
Producer: 20140304
In:
Journal of medicinal chemistry vol. 56
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Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach. [electronic resource] by
- Innocenti, Paolo
- Woodward, Hannah L
- Solanki, Savade
- Naud, Sébastien
- Westwood, Isaac M
- Cronin, Nora
- Hayes, Angela
- Roberts, Jennie
- Henley, Alan T
- Baker, Ross
- Faisal, Amir
- Mak, Grace Wing-Yan
- Box, Gary
- Valenti, Melanie
- De Haven Brandon, Alexis
- O'Fee, Lisa
- Saville, Harry
- Schmitt, Jessica
- Matijssen, Berry
- Burke, Rosemary
- van Montfort, Rob L M
- Raynaud, Florence I
- Eccles, Suzanne A
- Linardopoulos, Spiros
- Blagg, Julian
- Hoelder, Swen
Producer: 20170718
In:
Journal of medicinal chemistry vol. 59
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35.
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Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N [electronic resource] by
- Woodward, Hannah L
- Innocenti, Paolo
- Cheung, Kwai-Ming J
- Hayes, Angela
- Roberts, Jennie
- Henley, Alan T
- Faisal, Amir
- Mak, Grace Wing-Yan
- Box, Gary
- Westwood, Isaac M
- Cronin, Nora
- Carter, Michael
- Valenti, Melanie
- De Haven Brandon, Alexis
- O'Fee, Lisa
- Saville, Harry
- Schmitt, Jessica
- Burke, Rosemary
- Broccatelli, Fabio
- van Montfort, Rob L M
- Raynaud, Florence I
- Eccles, Suzanne A
- Linardopoulos, Spiros
- Blagg, Julian
- Hoelder, Swen
Producer: 20191014
In:
Journal of medicinal chemistry vol. 61
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36.
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C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays. [electronic resource] by
- Le Bihan, Yann-Vaï
- Lanigan, Rachel M
- Atrash, Butrus
- McLaughlin, Mark G
- Velupillai, Srikannathasan
- Malcolm, Andrew G
- England, Katherine S
- Ruda, Gian Filippo
- Mok, N Yi
- Tumber, Anthony
- Tomlin, Kathy
- Saville, Harry
- Shehu, Erald
- McAndrew, Craig
- Carmichael, LeAnne
- Bennett, James M
- Jeganathan, Fiona
- Eve, Paul
- Donovan, Adam
- Hayes, Angela
- Wood, Francesca
- Raynaud, Florence I
- Fedorov, Oleg
- Brennan, Paul E
- Burke, Rosemary
- van Montfort, Rob L M
- Rossanese, Olivia W
- Blagg, Julian
- Bavetsias, Vassilios
Producer: 20190725
In:
European journal of medicinal chemistry vol. 177
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37.
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Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. [electronic resource] by
- Reader, John C
- Matthews, Thomas P
- Klair, Suki
- Cheung, Kwai-Ming J
- Scanlon, Jane
- Proisy, Nicolas
- Addison, Glynn
- Ellard, John
- Piton, Nelly
- Taylor, Suzanne
- Cherry, Michael
- Fisher, Martin
- Boxall, Kathy
- Burns, Samantha
- Walton, Michael I
- Westwood, Isaac M
- Hayes, Angela
- Eve, Paul
- Valenti, Melanie
- de Haven Brandon, Alexis
- Box, Gary
- van Montfort, Rob L M
- Williams, David H
- Aherne, G Wynne
- Raynaud, Florence I
- Eccles, Suzanne A
- Garrett, Michelle D
- Collins, Ian
Producer: 20120308
In:
Journal of medicinal chemistry vol. 54
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Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737). [electronic resource] by
- Osborne, James D
- Matthews, Thomas P
- McHardy, Tatiana
- Proisy, Nicolas
- Cheung, Kwai-Ming J
- Lainchbury, Michael
- Brown, Nathan
- Walton, Michael I
- Eve, Paul D
- Boxall, Katherine J
- Hayes, Angela
- Henley, Alan T
- Valenti, Melanie R
- De Haven Brandon, Alexis K
- Box, Gary
- Jamin, Yann
- Robinson, Simon P
- Westwood, Isaac M
- van Montfort, Rob L M
- Leonard, Philip M
- Lamers, Marieke B A C
- Reader, John C
- Aherne, G Wynne
- Raynaud, Florence I
- Eccles, Suzanne A
- Garrett, Michelle D
- Collins, Ian
Producer: 20170606
In:
Journal of medicinal chemistry vol. 59
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Achieving [electronic resource] by
- Bellenie, Benjamin R
- Cheung, Kwai-Ming J
- Varela, Ana
- Pierrat, Olivier A
- Collie, Gavin W
- Box, Gary M
- Bright, Michael D
- Gowan, Sharon
- Hayes, Angela
- Rodrigues, Matthew J
- Shetty, Kartika N
- Carter, Michael
- Davis, Owen A
- Henley, Alan T
- Innocenti, Paolo
- Johnson, Louise D
- Liu, Manjuan
- de Klerk, Selby
- Le Bihan, Yann-Vaï
- Lloyd, Matthew G
- McAndrew, P Craig
- Shehu, Erald
- Talbot, Rachel
- Woodward, Hannah L
- Burke, Rosemary
- Kirkin, Vladimir
- van Montfort, Rob L M
- Raynaud, Florence I
- Rossanese, Olivia W
- Hoelder, Swen
Producer: 20200924
In:
Journal of medicinal chemistry vol. 63
Availability: No items available.
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40.
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8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. [electronic resource] by
- Bavetsias, Vassilios
- Lanigan, Rachel M
- Ruda, Gian Filippo
- Atrash, Butrus
- McLaughlin, Mark G
- Tumber, Anthony
- Mok, N Yi
- Le Bihan, Yann-Vaï
- Dempster, Sally
- Boxall, Katherine J
- Jeganathan, Fiona
- Hatch, Stephanie B
- Savitsky, Pavel
- Velupillai, Srikannathasan
- Krojer, Tobias
- England, Katherine S
- Sejberg, Jimmy
- Thai, Ching
- Donovan, Adam
- Pal, Akos
- Scozzafava, Giuseppe
- Bennett, James M
- Kawamura, Akane
- Johansson, Catrine
- Szykowska, Aleksandra
- Gileadi, Carina
- Burgess-Brown, Nicola A
- von Delft, Frank
- Oppermann, Udo
- Walters, Zoe
- Shipley, Janet
- Raynaud, Florence I
- Westaway, Susan M
- Prinjha, Rab K
- Fedorov, Oleg
- Burke, Rosemary
- Schofield, Christopher J
- Westwood, Isaac M
- Bountra, Chas
- Müller, Susanne
- van Montfort, Rob L M
- Brennan, Paul E
- Blagg, Julian
Producer: 20160726
In:
Journal of medicinal chemistry vol. 59
Availability: No items available.
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